PH12016501470B1 - Crystalline forms of an androgen receptor modulator - Google Patents
Crystalline forms of an androgen receptor modulatorInfo
- Publication number
- PH12016501470B1 PH12016501470B1 PH12016501470A PH12016501470A PH12016501470B1 PH 12016501470 B1 PH12016501470 B1 PH 12016501470B1 PH 12016501470 A PH12016501470 A PH 12016501470A PH 12016501470 A PH12016501470 A PH 12016501470A PH 12016501470 B1 PH12016501470 B1 PH 12016501470B1
- Authority
- PH
- Philippines
- Prior art keywords
- androgen receptor
- receptor modulator
- crystalline forms
- modulator
- trifluoromethylpyridin
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4184—1,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/08—Drugs for disorders of the urinary system of the prostate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P15/00—Drugs for genital or sexual disorders; Contraceptives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P33/00—Antiparasitic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
- A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
- A61P5/28—Antiandrogens
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Tropical Medicine & Parasitology (AREA)
- Urology & Nephrology (AREA)
- Reproductive Health (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicinal Preparation (AREA)
Abstract
Described herein are amorphous and crystalline forms of the androgen receptor modulator 4-[7-(6-cyano-5-trifluoromethylpyridin-3-yl)-8-oxo-6-thioxo-5,7-diazaspiro[3.4]oct-5-yl]-2-fluoro-N-methylbenzamide. Also described are pharmaceutical compositions suitable for administration to a mammal that include the androgen receptor modulator, and methods of using the androgen receptor modulator, alone and in combination with other compounds, for treating diseases or conditions that are associated with androgen receptor activity.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261656888P | 2012-06-07 | 2012-06-07 | |
| PCT/US2013/044116 WO2013184681A1 (en) | 2012-06-07 | 2013-06-04 | Crystalline forms of an androgen receptor modulator |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| PH12016501470A1 PH12016501470A1 (en) | 2017-07-10 |
| PH12016501470B1 true PH12016501470B1 (en) | 2021-12-10 |
Family
ID=49712550
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12014502714A PH12014502714B1 (en) | 2012-06-07 | 2014-12-04 | Crystalline forms of an androgen receptor modulator |
| PH12016501470A PH12016501470B1 (en) | 2012-06-07 | 2016-07-26 | Crystalline forms of an androgen receptor modulator |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PH12014502714A PH12014502714B1 (en) | 2012-06-07 | 2014-12-04 | Crystalline forms of an androgen receptor modulator |
Country Status (45)
Families Citing this family (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008119015A2 (en) | 2007-03-27 | 2008-10-02 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
| PE20150099A1 (en) | 2011-12-16 | 2015-01-30 | Olema Pharmaceuticals Inc | NOVELTY BENZOPYRAN COMPOUNDS, COMPOSITIONS AND USES OF THEM |
| ES2809738T3 (en) | 2012-06-07 | 2021-03-05 | Aragon Pharmaceuticals Inc | Crystalline forms of an androgen receptor modulator |
| WO2014043208A1 (en) | 2012-09-11 | 2014-03-20 | Medivation Prostate Therapeutics, Inc. | Formulations of enzalutamide |
| PT3305285T (en) | 2012-09-26 | 2020-11-24 | Aragon Pharmaceuticals Inc | Anti-androgens for the treatment of non-metastatic castrate-resistant prostate cancer |
| JOP20200097A1 (en) | 2013-01-15 | 2017-06-16 | Aragon Pharmaceuticals Inc | Androgen receptor modulator and uses thereof |
| CN106795152B (en) * | 2014-08-26 | 2020-01-31 | 安斯达尔生物技术有限责任公司 | protein kinase inhibitor |
| CR20170217A (en) | 2014-12-05 | 2017-08-30 | Aragon Pharmaceuticals Inc | ANTI-TARGET COMPOSITIONS |
| CA2969675C (en) | 2014-12-05 | 2023-06-06 | Aragon Pharmaceuticals, Inc. | Anticancer compositions |
| BR112017011788A2 (en) | 2014-12-05 | 2017-12-26 | Aragon Pharmaceuticals Inc | anticancer compositions |
| WO2016100905A1 (en) | 2014-12-19 | 2016-06-23 | Lutron Electronics Co., Inc. | Multi-channel lighting fixture having multiple light-emitting diode drivers |
| TW201808287A (en) | 2016-06-03 | 2018-03-16 | 美商艾瑞岡醫藥公司 | Anticancer compositions |
| ES2952770T3 (en) | 2016-12-13 | 2023-11-06 | Watson Lab Inc | Solid State Forms of Apalutamide |
| EP4438126A3 (en) | 2017-10-16 | 2025-01-01 | Aragon Pharmaceuticals, Inc. | Anti-androgens for the treatment of non-metastatic castration-resistant prostate cancer |
| WO2019135254A1 (en) | 2018-01-02 | 2019-07-11 | Mylan Laboratories Limited | Apalutamide polymorphs and their preparation thereof |
| WO2019242439A1 (en) * | 2018-06-20 | 2019-12-26 | 苏州科睿思制药有限公司 | Crystal form of arn-509, preparation method therefor and use thereof |
| WO2020049598A2 (en) | 2018-09-08 | 2020-03-12 | Cipla Limited | Apalutamide polymorphs |
| IT201900003839A1 (en) | 2019-03-15 | 2020-09-15 | Olon Spa | STABLE AMORPHOUS APALUTAMIDE SYNTHESIS |
| WO2020234817A1 (en) * | 2019-05-21 | 2020-11-26 | Laurus Labs Limited | Polymorphic forms of apalutamide and its preparation thereof |
| IT201900010593A1 (en) | 2019-07-01 | 2021-01-01 | Dipharma Francis Srl | CRYSTALLINE FORM OF AN ANDROGEN RECEPTOR INHIBITOR |
| EP4017848A1 (en) * | 2019-08-22 | 2022-06-29 | Dr. Reddy's Laboratories Ltd. | Process for the preparation of apalutamide |
| IT201900015974A1 (en) | 2019-09-10 | 2021-03-10 | Olon Spa | STABLE CRYSTALLINE APALUTAMIDE IN PURE FORM AND PROCESS FOR ITS PREPARATION |
| CN110590740A (en) * | 2019-09-20 | 2019-12-20 | 武汉大学 | A kind of apalutamide compound and its pharmaceutical preparation |
| WO2022049265A1 (en) | 2020-09-04 | 2022-03-10 | Synthon B.V. | Improved process for preparation of apalutamide |
| CN112679468A (en) * | 2021-01-05 | 2021-04-20 | 四川科伦药物研究院有限公司 | Crystal form of apatamide, preparation method and application |
| WO2023143090A1 (en) * | 2022-01-25 | 2023-08-03 | 成都苑东生物制药股份有限公司 | Novel crystalline form of apalutamide solvate and preparation method therefor |
| CN115536634B (en) * | 2022-10-17 | 2024-06-11 | 上海博悦生物科技有限公司 | Synthesis method of apatamide |
| CN116332907A (en) * | 2023-03-16 | 2023-06-27 | 奥锐特药业股份有限公司 | A kind of preparation method of amorphous apalutamide |
| WO2025153768A1 (en) * | 2024-01-18 | 2025-07-24 | Nanoform Finland Oyj | Composition comprising crystalline nanosized apalutamide |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5323907A (en) | 1992-06-23 | 1994-06-28 | Multi-Comp, Inc. | Child resistant package assembly for dispensing pharmaceutical medications |
| US7709517B2 (en) | 2005-05-13 | 2010-05-04 | The Regents Of The University Of California | Diarylhydantoin compounds |
| CN101032483B (en) * | 2006-03-09 | 2011-05-04 | 陈德桂 | Hydantoin derivative for adjusting estrogen receptor activity and application thereof |
| PL3412290T3 (en) | 2006-03-27 | 2021-09-06 | The Regents Of The University Of California | Androgen receptor modulator for the treatment of prostate cancer and androgen receptor-associated diseases |
| CA2648139A1 (en) * | 2006-03-29 | 2007-11-08 | The Regents Of The University Of California | Diaryl thiohydantoin compounds and their use in the treatment of hyperproliferative disorders |
| WO2008119015A2 (en) * | 2007-03-27 | 2008-10-02 | Sloan-Kettering Institute For Cancer Research | Synthesis of thiohydantoins |
| EA028869B1 (en) | 2010-02-16 | 2018-01-31 | Арагон Фармасьютикалс, Инк. | Androgen receptor modulators and use thereof |
| ES2809738T3 (en) | 2012-06-07 | 2021-03-05 | Aragon Pharmaceuticals Inc | Crystalline forms of an androgen receptor modulator |
| WO2019242439A1 (en) | 2018-06-20 | 2019-12-26 | 苏州科睿思制药有限公司 | Crystal form of arn-509, preparation method therefor and use thereof |
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2013
- 2013-06-04 ES ES18157435T patent/ES2809738T3/en active Active
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- 2013-06-04 CA CA3055660A patent/CA3055660A1/en not_active Abandoned
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2014
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2015
- 2015-01-06 ZA ZA2015/00076A patent/ZA201500076B/en unknown
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2016
- 2016-07-26 PH PH12016501470A patent/PH12016501470B1/en unknown
- 2016-09-12 US US15/262,522 patent/US9994545B2/en active Active
- 2016-12-19 HK HK16114389.2A patent/HK1226066A1/en unknown
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2017
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2018
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2019
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2020
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2021
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2024
- 2024-05-13 US US18/662,345 patent/US20250092011A1/en not_active Abandoned
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